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製品番号: HY-11073

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MK-0489

MK-0489 is an orally active, highly effective, and selective MC4R agonist. MK-0489 exhibits a strong binding affinity (IC₅₀ = 13 nM) and functional agonist activity (EC₅₀ = 4.6 nM) at human MC4R. MK-0489 shows functional activity of 22 nM (EC₅₀) on mouse MC4R and 1.7 μM (EC₅₀) on mouse MC3R. MK-0489 can be used for the study of obesity.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 778625-65-3
分子式: C₃₄H₄₄ClF₂N₃O₂
分子量:600.18

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

MK-0489 構造式

CAS 番号: 778625-65-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

MC4R

Melanocortin Receptor アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	1020 nM Compound: 1	Agonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	EC₅₀	1020 nM Compound: 1r, MK-0489	Agonist activity at human MC1bR expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins Agonist activity at human MC1bR expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	[PMID: 20598882]
CHO	EC₅₀	2 nM Compound: 1	Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	EC₅₀	22 nM Compound: 1	Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	EC₅₀	351 nM Compound: 1	Agonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	EC₅₀	4.6 nM Compound: 1r, MK-0489	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	[PMID: 20598882]
CHO	EC₅₀	4.9 nM Compound: 1	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	EC₅₀	997 nM Compound: 1	Agonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	IC₅₀	13 nM Compound: 1	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	[PMID: 20207541]
CHO	IC₅₀	13 nM Compound: 1r, MK-0489	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	[PMID: 20598882]
CHO	IC₅₀	1938 nM Compound: 1	Displacement of [125I]NDP-alpha-MSH from human MC1R expressed in CHO cells Displacement of [125I]NDP-alpha-MSH from human MC1R expressed in CHO cells	[PMID: 20207541]
CHO	IC₅₀	83.9 nM Compound: 1	Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells	[PMID: 20207541]
CHO	IC₅₀	890 nM Compound: 1	Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells	[PMID: 20207541]

体内実験

MK-0489 (Compound 1r) (2-20 mg/kg, p.o., once or twice daily for 14 days) specifically reduces food intake and body weight in mice via MC4R-mediated reduction, and in a dose-dependent manner, it reduces body weight in a diet-induced obese rat model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Wild type (WT) and MC4R/3R knockout (KO) mouse^[1].
Dosage:

10 mg/kg
Administration:

P.o., once
Result:

Significant reducted in food intake and body weight was observed in wild-type mice; however, no significant effect was observed in MC4R/3R knockout mice.

Animal Model:

Diet-induced obese rat model^[1].
Dosage:

2 mg/kg, 6 mg/kg, 20 mg/kg
Administration:

P.o., twice a day for 14 days
Result:

Exhibited dose-dependent weight loss effect.

化学情報

CAS 番号 778625-65-3
分子量 600.18
分子式 C₃₄H₄₄ClF₂N₃O₂
SMILES

CC(NC(C)([C@@H]1CC2(CCN(C([C@@H]3CN(C(C)(C)C)C[C@H]3C4=CC=C(F)C=C4F)=O)CC2)C5=C1C=C(C)C(Cl)=C5)C)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (276 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. He S, et al. Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4399-405. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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MK-0489

Melanocortin Receptor アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

MK-0489 関連分類

HY-11073 関連分類